The present invention relates to opiate derived compositions and their antagonists useful in therapeutic areas associated with opioid receptor modulation. A 3-hexadienoate modification of the opioids is formulated to improve opiates' engagement of the opioid receptors when given orally. A 3-hexadienoate modification of nalbuphine or a pharmaceutically acceptable salt of thereof to improve quality of pain management when given intravenously, intranasally, transdermally, sublingually, rectally, topically, intramuscularly, subcutaneously or via inhalation. A 3-hexadienoate modification of the opioids antagonists is formulated to improve inhibition of the opioid receptors when given orally. A 3-hexadienoate modification of naloxone or a pharmaceutically acceptable salt of thereof to improve quality of Sobering when given intravenously, intranasally, transdermally, sublingually, rectally, topically, intramuscularly, subcutaneously or via inhalation.

Disclosed are methods for preparing buprenorphine from, for example, compounds such as nororipavine and northebaine.

Provided is a cost-effective process for preparing naldemedine having high purity with high yields.

Provided is a cost-effective process for preparing naldemedine having high purity with high yields.

This invention relates to opioid ketal compounds of Formula (I), Formula (II), or Formula (III): or a pharmaceutically acceptable salts thereof, wherein R.sub.1 is H or CH.sub.3, R.sub.2 is H or OH, n is 0, 1, 2 or 3, R.sub.3 and R.sub.4 are independently H or optionally substituted C.sub.1-C.sub.4 alkyl, or when n is 0, then R.sub.3 and R.sub.4 and the carbon atoms to which they are attached together form six, or seven membered ring, which is optionally mono or disubstituted by C.sub.1-C.sub.4 alkyl. The invention also relates to oxycodone ketal compounds of Formula (IV) or (V): or a pharmaceutically acceptable salts thereof. The invention also relates to the use of such compounds for the treatment, prevention, or amelioration of pain. ##STR00001##

This invention relates to opioid ketal compounds of Formula (I), Formula (II), or Formula (III): or a pharmaceutically acceptable salts thereof, wherein R.sub.1 is H or CH.sub.3, R.sub.2 is H or OH, n is 0, 1, 2 or 3, R.sub.3 and R.sub.4 are independently H or optionally substituted C.sub.1-C.sub.4 alkyl, or when n is 0, then R.sub.3 and R.sub.4 and the carbon atoms to which they are attached together form six, or seven membered ring, which is optionally mono or disubstituted by C.sub.1-C.sub.4 alkyl. The invention also relates to oxycodone ketal compounds of Formula (IV) or (V): or a pharmaceutically acceptable salts thereof. The invention also relates to the use of such compounds for the treatment, prevention, or amelioration of pain. ##STR00001##

The present invention relates to an opioid receptor antagonist conjugate and a use thereof. In particular, the present invention relates to a covalent coupling conjugate of a hydrophilic polymer and an opioid receptor antagonist and the use thereof.

The present invention relates to an opioid receptor antagonist conjugate and a use thereof. In particular, the present invention relates to a covalent coupling conjugate of a hydrophilic polymer and an opioid receptor antagonist and the use thereof.

The present invention relates to opiate derived compositions and their antagonists useful in therapeutic areas associated with opioid receptor modulation. A 3-hexadienoate modification of the opioids is formulated to improve opiates' engagement of the opioid receptors when given orally. A 3-hexadienoate modification of Nalbuphine or a pharmaceutically acceptable salt of thereof to improve quality of pain management when given intravenously, intranasally, transdermally, sublingually, rectally, topically, intramuscularly, subcutaneously or via inhalation. A 3-hexadienoate modification of the opioids antagonists is formulated to improve inhibition of the opioid receptors when given orally. A 3-hexadienoate modification of Naloxone or a pharmaceutically acceptable salt of thereof to improve quality of Sobering when given intravenously, intranasally, transdermally, sublingually, rectally, topically, intramuscularly, subcutaneously or via inhalation.

The present invention related to novel morphinans, compositions comprising the novel morphinans, and their uses as agonists of the kappa opioid receptor.